Development and Evaluation of Sildenafil Citrate Tablet Fabricated by Direct Compression Method
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Abstract
The objective of this research was to develop the formulas of sildenafil citrate tablet, normally used to treat erectile dysfunction diseases. The tablets were prepared by direct compression method. Each tablet consisted of the sildenafil citrate (equivalence to 10 mg of sildenafil), direct compression excipients as spray dried lactose (SDL) or microcrystalline cellulose (MCC) or combination of SDL with MCC in a ratio of 1: 1, glidants as 0.2% of colloidal silicon dioxide and lubricants as 1% of magnesium stearate. These formulations were evaluated for powder properties. Each formulations were compressed to crushing strength (CS) at 4 and 8 kgf at 100 mg per tablet. These tablets were evaluated for tablet quality. The results showed that the formulation contained SDL had excellent powder flow properties. The formulation contained SDL: MCC (1: 1) had powder flow properties better than that using only MCC. Each formulation met the acceptance criteria of weight variation and uniformity of dosage units in the pharmacopoeia. The tablets used MCC had low friability (F) and disintegration time (DT). The tablets used combination of SDL: MCC (1: 1) exhibited lower F and DT than those using only SDL. These tablets, compressed to CS 8 kgf appeared higher crushing strength/friability ratio (CSFR) than those of 4 kgf tablets, whereas a CSFR/DT was lower than that of 4 kgf tablets. Drug Release of sildenafil citrate from tablets used MCC and SDL: MCC (1: 1) at CS 4 and 8 kgf at 15 min were greater than 80% and met the standard requirement of dissolution test in the pharmacopoeia. It can be concluded that direct compressed tablet of sildenafil citrate consisting of the MCC or SDL: MCC (1: 1), colloidal silicon dioxide, and magnesium stearate, and then compressed to CS 4 and 8 kgf are complied with the United States Pharmacopeia (USP 40/NF 35) and might be used as guidance for development of low-dose formulation of tablets for safe treatment and reducing side effects from high-dose tablet.
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References
Ayorinde JO, Odeniyi MA, Itiola AO. Evaluation of Pharmaceutical and Chemical Equivalence Selected Brands of Diclofenac Sodium Tablets. East Cent Afr J Pharm Sci 2012; 15: 3-9.
Christiansen E, Guirguis WR, Cox D, Osterloh IH. Long-Term Efficacy and Safety of Oral Viagra (Sildenafil Citrate) in Men with Erectile Dysfunction and the Effect of Randomised Treatment Withdrawal. Int J Important Res 2000; 12: 177-182.
Jones DS. Solid-dosage forms: tablets. In: Jones DS, editors. Pharmaceutics-Dosage Form and Design. Pharmaceuticcal Press. London. 2008. 286.
Kanokwan J, Jomjai P, Sukanya P. Development of Analytical Determination of Sildenafil Citrate Tablet. Isan J Pharm Sci 2006; 2(2): 1-8.
Kim G. The Effect of Crystalline and Amorphous Lactose on Mechanical of Roller Compaction Ribbon and Tablets (Dissertation). Lawrence, USA, University of Kansas; 2014. 56p.
Morales AM, Mirone V, Dean J, Costa P. Varidenafil for The Treatment of Erectile Dysfunction: An Overview of The Clinical Evidence. Clin Intervention Aging 2009; 4: 463-472.
Pedro IDR, Brandao ICC, Souza GMCP, Carneiro G. Development of Tablet Formulations of Calcium Carbonate by Direct Compression. J Appl Pharm Sci 2017; 4(2): 12-20.
Rasha KD, Myasar A-K. Formulation of Orally Disintegrating Tablets of Cinnarizine by using Direct Compression Method. Int J Appl Pharm 2019; 11(1): 117-123.
Sunee C, Tawatchai T, Pathamaporn C. Development of Mannitol-Corn Starch Co-processed Direct Compression Excipient Using Lactitol as Binder. Isan J Pharm Sci 2017; 13(4): 63-76.
Søgaard SV, Bryder M, Allesø M, Rantanen J. Characterization of powder properties using a powder rheometer. MDPI AG [online] 2012 Apr 30 [cited 2019 Apr 27]. Available at: https://sciforum.net/paper/view/conference/825
The United States Pharmacopoeia 40/National Formulary 35. Rockville: The United States Pharmacopoeia Convention, 2017. 802-805, 6156-6159.
Worranan R, Penpun W, Prasert A, Praneet O, Nattawat N. Development of High Active Andrographolide Tablet from Andrographis Paniculata Extract. Thai J Pharm Sci 2018; 42(Suppl.): 223-226.
Yanisa B, Saengrawee S, Padungkwan C. A Feasibility Study of Alcoholic-Alkaline Treated Rice Starch for Disintegrant in Tablet. In: Graduate School, Khon Kaen University, editors. GRC 2013: Proceedings of the 14th Graduate Research Conference; 2013 Feb 22; Khon Kaen. Thailand: 2013. p.1069-1077.
Young JM, Bennett C, Gilhooly P, Wessells H, Ramos DE. Efficacy and Safety of Sildenafil Citrate (Viagra) in Black and Hispanic American Men. Urology 2002; 60(2 Suppl 2): 39-48.